Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.

Article Details

Citation
Copy to clipboard

Tamiya J, Dyck B, Zhang M, Phan K, Fleck BA, Aparicio A, Jovic F, Tran JA, Vickers T, Grey J, Foster AC, Chen C

Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3328-32. doi: 10.1016/j.bmcl.2008.04.025. Epub 2008 Apr 15.

PubMed ID
18445525 [ View in PubMed
]
Abstract

A series of milnacipran analogs were synthesized and studied as monoamine transporter inhibitors, and several potent compounds with moderate lipophilicity were identified from the 1S,2R-isomers. Thus, 15l exhibited IC(50) values of 1.7nM at NET and 25nM at SERT, which were, respectively, 20- and 13-fold more potent than 1S,2R-milnacipran 1-II.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AtomoxetineSodium-dependent noradrenaline transporterIC 50 (nM)5.1N/AN/ADetails
AtomoxetineSodium-dependent serotonin transporterIC 50 (nM)190N/AN/ADetails
LevomilnacipranSodium-dependent noradrenaline transporterIC 50 (nM)77N/AN/ADetails
LevomilnacipranSodium-dependent noradrenaline transporterIC 50 (nM)40N/AN/ADetails
LevomilnacipranSodium-dependent serotonin transporterIC 50 (nM)420N/AN/ADetails
LevomilnacipranSodium-dependent serotonin transporterIC 50 (nM)320N/AN/ADetails
MilnacipranSodium-dependent noradrenaline transporterIC 50 (nM)5500N/AN/ADetails
MilnacipranSodium-dependent serotonin transporterIC 50 (nM)3500N/AN/ADetails